CDC策略下三氯化铁催化哒嗪酮衍生物N-H烷基化研究

Research on FeCl_(3)-catalyzed N-H Alkylation of Pyridazinone Derivatives via the CDC Strategy

利用FeCl_(3)催化的交叉脱氢偶联反应,在温和反应条件下,建立了哒嗪酮N-H与烷基C(sp^(3))-H之间形成C-N键的方法.不同的哒嗪酮类化合物与氧/硫醚反应,顺利得到了一系列N-氧基/硫烷基哒嗪酮衍生物,收率为44%~83%.该方法为构建具有潜在生物活性的N-取代哒嗪酮类化合物提供了一种新的策略.

A method for the formation of a C-N bond between pyridazinone N-H and alkylic C(sp^(3))-H through FeCl,catalyzed cross dehydrogenative coupling was developed under mild reaction conditions.Various pyridazinones could react smoothly with oxy/thioethers to provide the N-oxy/thioalkyl pyridazinone derivatives with moderate to good yields(44%~83%).This method provides an alternative tactic to construct potentially bioactive N-substituted pyridazinones.